Saquinavir

Saquinavir is a prescription medication used to treat human immunodeficiency virus (HIV) infection, which causes acquired immunodeficiency syndrome (AIDS).

• Saquinavir is available under the following different brand names: Invirase

Common side effects of Saquinavir include:

• diarrhea
• nausea
• vomiting
• stomach pain
• tiredness
• changes in the shape or location of body fat (especially in your arms, legs, face, neck, breasts, and waist)

Serious side effects of Saquinavir include:

• stabbing chest pain
• fever
• infection
• rapid heart rate
• weakness
• trouble breathing or swallowing

Rare side effects of Saquinavir include:

• none

Seek medical care or call 911 at once if you have the following serious side effects:

• Severe headache, confusion, slurred speech, arm or leg weakness, trouble walking, coordination loss, unsteady, very stiff muscles, high fever, profuse sweating, or tremors.
• Serious eye symptoms such as sudden vision loss, blurred vision, tunnel vision, eye pain or swelling, or seeing halos around lights.
• Serious heart symptoms include fast, irregular, or pounding heartbeats; fluttering in the chest; shortness of breath; sudden dizziness, lightheadedness, or passing out.

This is not a complete list of side effects and other serious side effects or health problems that may occur because of the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may report side effects or health problems to FDA at 1-800-FDA-1088.

Adult and pediatric dosage

Tablet

• 500 mg

HIV Infection

Adult dosage

• 1000 mg (with ritonavir 100 mg) orally every 12 hours, or in combination with ritonavir-enhanced lopinavir
• Treatment-naive patients
  • Initial dose: 500 mg orally two times a day plus ritonavir 100 mg two times a day for 7 days; then increase the dose to 1000 mg/100 mg orally two times a day.
  • This gradual increase is due to the potential for increased risk for PR and QT interval prolongation with the standard 1000 mg/100 mg dose two times a day
  • For patients with a baseline QT interval below 450 msec, an on-treatment ECG is recommended after approximately 10 days of therapy
  • Patients with a QT interval prolongation over pretreatment by above 20 msec should discontinue Saquinavir/ritonavir therapy

Pediatric dosage

• Children aged younger than 16 years: Safety and efficacy not established.
• Children aged 16 years and older: 1000 mg (plus ritonavir 100 mg) orally every 12 hours.
• For patients already taking ritonavir 100 mg two times a day as part of their ART regimen, no additional ritonavir is needed.
• Treatment-naive patients
  • Initial dose: 500 mg orally two times a day plus ritonavir 100 mg two times a day for 7 days; then increase to 1000 mg/100 mg orally two times a day
  • This gradual increase is due to the potential for increased risk for PR and QT interval prolongation with standard 1000 mg/100 mg two times a day dose
  • For patients with a baseline QT interval below 450 msec, an on-treatment ECG is recommended after approximately 10 days of therapy
  • Patients with a QT interval prolongation over pretreatment by above 20 msec should discontinue Saquinavir/ritonavir therapy
• Investigational in treatment-experienced children
  • Children aged below 2 years: Safety and efficacy not established.
  • Children aged 2 years and older, weighing between 5 to 14 kg: 50 mg/kg (plus ritonavir 3 mg/kg) orally every 12 hours.  
  • Children aged 2 years and older, and weighing between 15 to 40 kg: 50 mg/kg (plus ritonavir 2.5 mg/kg) orally every 12 hours.
  • Children aged 2 years and older, and weighing 40 kg and more: 50 mg/kg (plus ritonavir 100mg) orally every 12 hours.

Dosage Considerations – Should be Given as Follows: 

• See “Dosages”

If your medical doctor is using this medicine to treat your pain, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, healthcare provider, or pharmacist first.

• Saquinavir has severe interactions with at least 60 other drugs.
• Saquinavir has serious interactions with at least 241 other drugs.
• Saquinavir has moderate interactions with at least 342 other drugs.
• Saquinavir has minor interactions with the following drugs:
  • acetazolamide
  • anastrozole
  • cilostazol
  • cyclophosphamide
  • food
  • ganaxolone
  • ixazomib
  • paclitaxel
  • paclitaxel protein-bound

This information does not contain all possible interactions or adverse effects. Visit the RxList Drug Interaction Checker for any drug interactions. Therefore, before using this product, tell your doctor or pharmacist about all the products you use. Keep a list of all your medications with you and share this information with your doctor and pharmacist. Check with your healthcare professional or doctor for additional medical advice, health questions, or concerns.

Contraindications

• Hypersensitivity (e.g., anaphylactic reactions, Stevens-Johnson syndrome)
• An ECG should be performed before initiation of treatment; patients with a QT interval equal to 450 msec should not initiate therapy
• Treatment-naïve patients initiating therapy should receive a reduced starting dose of saquinavir 500 mg twice daily with ritonavir 100 mg twice daily for the first 7 days of treatment followed by Saquinavir/ritonavir 1000 mg/100 mg twice daily due to the potential for an increased risk for PR and QT interval prolongation with the standard 1000 mg/100 mg twice daily dose
• QT and PR interval prolongation and torsades de pointes have been reported rarely; do not use saquinavir/ritonavir with congenital or documented acquired QT prolongation (450 msec and more), refractory hypokalemia, or hypomagnesemia, and in combination with drugs that prolong QT interval
• Complete atrioventricular (AV) block without implanted pacemakers or high risk for complete AV block
• Severe hepatic impairment
  • Coadministration of saquinavir/ritonavir with rifampin due to the risk of severe hepatotoxicity
  • Drugs that are contraindicated with saquinavir (when coadministered 'boosted' with ritonavir) include CYP3A inhibitors, which may result in increased Saquinavir plasma levels and cause serious or life-threatening reactions (e.g., prolonged QT interval)
  • Drugs contraindicated with saquinavir/ritonavir include alfuzosin, antiarrhythmics (amiodarone, bepridil, flecainide, propafenone, quinidine, lidocaine), trazodone, rifampin, voriconazole, ergot derivatives (dihydroergotamine, ergonovine, ergotamine, methylergonovine), cisapride, St. John’s wort, HMG-CoA reductase inhibitors (lovastatin, simvastatin), lurasidone, pimozide, clarithromycin, erythromycin, halofantrine, pentamidine, clozapine, haloperidol, sertindole, ziprasidone, atazanavir, tacrolimus, rilpivirine, dasatinib, sunitinib, disopyramide, quinine, phenothiazines (eg, chlorpromazine, mesoridazine, thioridazine), sildenafil (when used for PAH), midazolam, and triazolam

Effects of drug abuse

• None

Short-Term Effects

• See “What Are Side Effects Associated with Using Saquinavir?”

Long-Term Effects

• See “What Are Side Effects Associated with Using Saquinavir?”

Cautions

• Hyperlipidemia may occur
• Take within 2 hours after a meal; absorption increased with a high-fat meal
• Must be used in combination with ritonavir (ie, boosted therapy) to achieve the necessary levels of effectiveness
• Autoimmune disorders (eg, Grave’s disease, polymyositis, Guillain-Barré syndrome) are reported in the setting of immune reconstitution; however, time to onset is variable and can occur many months after treatment initiation
• Risk for QT and PR prolongation that might lead to torsades de pointes (particularly if used with ritonavir); discontinue therapy if significant arrhythmia or QT/ PR prolongation occurs; perform ECG before initiation of treatment; patients with a baseline QT interval <450 msec, an on-treatment ECG is recommended after approximately 10 days of therapy; patients with a QT interval prolongation over pretreatment by above 20 msec should discontinue Saquinavir/ritonavir therapy
• May develop new onset or exacerbations of diabetes mellitus, hyperglycemia, elevated cholesterol and/or triglyceride concentrations, redistribution/accumulation of body fat, and immune reconstitution syndrome; monitor cholesterol and triglycerides before therapy and periodically thereafter
• In patients with underlying hepatitis B or C, cirrhosis, chronic alcoholism, or other underlying liver abnormalities, worsening of underlying liver disease and development of portal hypertension reported after initiating therapy; jaundice and exacerbation of chronic liver disease with grade 4 elevated liver function tests also observed; no dosage adjustment necessary for patients with mild or moderate hepatic impairment based on limited data; Saquinavir/ritonavir contraindicated in patients with severe hepatic impairment; if severe toxicity occurs during treatment, discontinue therapy
• Spontaneous bleeding may occur, and additional factor VII may be required
• Various degrees of cross-resistance have been observed
• Not recommended for use in combination with cobicistat
• Tablets and capsules contain lactose; not recommended in patients with rare hereditary problems of galactose intolerance, Lapp lactase deficiency, or glucose-galactose malabsorption

Pregnancy and Lactation

• There is a pregnancy exposure registry that monitors pregnancy outcomes in individuals exposed to antiretrovirals during pregnancy; healthcare providers are encouraged to register patients by calling the Antiretroviral Pregnancy Registry (APR) at 1-800-258-4263
• Prospective pregnancy data from the APR are not sufficient to adequately assess a drug-associated risk for birth defects or fetal outcomes; a limited number of reports on the use of the drugs during pregnancy has been submitted to the APR, and the number of exposures to drugs is insufficient to make the risk assessment compared to a reference population
• Lactation
  • The CDC recommends HIV-infected mothers in the US not to breastfeed their infants to avoid risking postnatal transmission of HIV-1
  • There are no data available regarding the presence of drugs in human milk, its effects on breastfed infants, or milk production
  • Because of the potential for HIV-1 transmission (in HIV-negative infants), developing viral resistance (in HIV-positive infants), and adverse reactions in breastfed infants like those seen in adults, instruct mothers not to breastfeed if receiving therapy